PLpro inhibitor 6, is a potent inhibitor of papain-like protease (PLpro) with an IC50 of 2.6 µM. PLpro inhibitor inhibits SARS-CoV-2 PLpro with an IC50 of 5.0 µM and an EC50 of 21.0 µM. KOM70144 has CAS#1093070-14-4, no formal name For the convenience of scientific communication, we named it as KOM70144 (combined from Inchi key plus CAS#) according to Hodoodo Chemical Nomenclature (https://hodoodo.com/hodoodo-chemical-nomenclature). KOM70144 was first reported by Kiira Ratia et al, Proc Natl Acad Sci U S A. 2008;105(42):16119-16124. (compound 6)
Chemical Formula: C22H22N2O2
Exact Mass: 346.1681
Molecular Weight: 346.43
Elemental Analysis: C, 76.28; H, 6.40; N, 8.09; O, 9.24
InChi Code: InChI=1S/C22H22N2O2/c1-14-11-12-18(24-16(3)25)13-21(14)22(26)23-15(2)19-10-6-8-17-7-4-5-9-20(17)19/h4-13,15H,1-3H3,(H,23,26)(H,24,25)/t15-/m1/s1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
PLpro inhibitor is a potent inhibitor against the papain-like protease (PLpro) from the coronavirus that causes severe acute respiratory syndrome (SARS-CoV). PLpro inhibitor was found to have IC50 value of 2.6 μM. PLpro inhibitor display significant antiviral activity with EC50 values of 13.1 μM, without toxicity up to the highest concentration tested. Notably, the increasing antiviral potency correlates with the in vitro inhibition of PLpro, suggesting that the compounds work directly on the enzyme in cells.
Characterization and Noncovalent Inhibition of the Deubiquitinase and deISGylase Activity of SARS-CoV-2 Papain-Like Protease Quick View Other Sources. By Freitas, Brendan T.; Durie, Ian A.; Murray, Jackelyn; Longo, Jaron E.; Miller, Holden C.; Crich, David; Hogan, Robert Jeff; Tripp, Ralph A.; Pegan, Scott D. From ACS Infectious Diseases (2020), Ahead of Print. |
Compositions and methods for identification, assessment, prevention, and treatment of AML using USP10 biomarkers and modulators. By Buhrlage, Sara; Weisberg, Ellen. From PCT Int. Appl. (2018), WO 2018057618 A1.
Compounds and methods for treating respiratory diseases. Ghosh, Arun K.; Takayama, Jun; Mesecar, Andrew David; Johnson, Michael E.; Ratia, Kiira M.; Chaudhuri, Rima; Mulhearn, Debbie C. From U.S. Pat. Appl. Publ. (2011), US 20110269834 A1.
Compounds and methods for treating respiratory diseases . By Ghosh, Arun K.; Takayama, Jun. From PCT Int. Appl. (2010), WO 2010022355 A1 20100225.
Ratia K, Pegan S, Takayama J, et al. A noncovalent class of papain-like protease/deubiquitinase inhibitors blocks SARS virus replication. Proc Natl Acad Sci U S A. 2008;105(42):16119-16124.
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